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Assay Detail

CHEMBL3821389

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of human recombinant His-tagged soluble COMT expressed in Escherichia coli BL21 using aesculetin as substrate after 60 mins by microplate assay in presence of SAM
6
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Catechol O-methyltransferase (CHEMBL2023)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of Potential Off-target Toxicity Liabilities of Catechol-O-methyltransferase Inhibitors by Differential Competition Capture Compound Mass Spectrometry.
von Kleist L, Michaelis S, Bartho K, Graebner O, Schlief M, Dreger M, Schrey AK, Sefkow M, Kroll F, Koester H, Luo Y.
J Med Chem (2016) 59 : 4664 -4675
PubMed 27074629 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.70 7.27
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3818719 1 7.27
CHEMBL1324 TOLCAPONE 4.0 1 6.90
CHEMBL3818350 1 6.75
CHEMBL953 ENTACAPONE 4.0 1 6.41
CHEMBL3819488 1 6.19
CHEMBL3818536 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3818719 IC50 = 54.0 nM 7.27
CHEMBL1324 TOLCAPONE IC50 = 127.0 nM 6.90
CHEMBL3818350 IC50 = 179.0 nM 6.75
CHEMBL953 ENTACAPONE IC50 = 386.0 nM 6.41
CHEMBL3819488 IC50 = 648.0 nM 6.19
CHEMBL3818536 Inhibition - % -